New Release: Alpha testing version has been released.

Crotamiton

D07X - Corticosteroids, other combinations ATC D07XA01 Unknown approved 1949 Topical

JFDA label: Crotaphil-H Cream

Mechanism of Action

— Unknown

Indications

Approved

  • Scabies

Contraindications

Source: Lexicomp

  • Hypersensitivity to crotamiton or any component of the formulation Absolute
  • patients who manifest a primary irritation response to topical medications Absolute

Adverse Reactions

Very Common >10%Common 1–10%Uncommon 0.1–1% Rare 0.01–0.1%Very Rare <0.01%Not Known

Nervous system disorders (1)

Not Known Localized warm feeling

Immune system disorders (1)

Not Known Local hypersensitivity reaction

Skin and subcutaneous tissue disorders (3)

Not Known Contact dermatitis · pruritus · skin rash

General disorders and administration site conditions (1)

Not Known Local irritation

Dosing

Source: Lexicomp

Pruritus: Topical: Massage into affected areas until medication is completely absorbed; repeat as necessary Scabies: Topical: Apply a thin layer and massage drug onto skin of the entire body from the neck to the toes (with special attention to skin folds, creases, and interdigital spaces). Repeat application in 24 hours. May re-treat if new lesions appear or itching persists more than 2 to 4 weeks after initial treatment (CDC 2010).
Refer to adult dosing.

Warnings & Precautions

Source: Lexicomp

Appropriate use

For external use only; avoid contact with face, eyes, mucous membranes, and urethral meatus. Do not apply to acutely inflamed, raw, or weeping skin. Discontinue use if severe irritation or sensitization occurs.

Pregnancy & Lactation

Pregnancy

FDA category C

Animal reproduction studies have not been conducted; use during pregnancy only if clearly needed.

Lactation

It is not known if crotamiton is excreted in breast milk.

Chemistry & Properties

2D structure
FormulaC13H17NO
Molecular weight203.28 g/mol
IUPAC nameN-ethyl-N-(2-methylphenyl)but-2-enamide
CAS483-63-6
PubChem CID2883
InChIKeyDNTGGZPQPQTDQF-UHFFFAOYSA-N
logP2.8 (XLogP 2.8)
Polar surface area20.3 Ų
H-bond acceptors / donors1 / 0
SMILESCCN(C1=CC=CC=C1C)C(=O)C=CC

Biology & Pharmacokinetics

Pharmacokinetics predicted

Bioavailability70.0%
Half-life0.631 h
Volume of distribution1.139 L/kg
Protein binding95.0%
BBB penetrantYes

Enzyme interactions

EnzymeRoleDetail
CYP1A2Substrate
CYP2B6Inhibitor
CYP2C19Substrate
CYP3A4Substrate

Transporters

BCRP (Inhibitor)BSEP (Inhibitor)MRP1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B1 (Inhibitor)OATP1B3 (Inhibitor)P-gp (Inhibitor)P-gp (Substrate)

Registered Products (1)

BrandForm / strengthPackAgentCitizen (JOD)
Crotaphil-H Cream Cream 10 %, 0.25 % 25 g tube PHILADELPHIA PHAEMACEUTICALS.COMP/JORDAN 1.820